EP1808176A3 - 5 alpha reduced glucocorticoid metabolites for the treatment of inflammation - Google Patents

5 alpha reduced glucocorticoid metabolites for the treatment of inflammation Download PDF

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Publication number
EP1808176A3
EP1808176A3 EP07004317A EP07004317A EP1808176A3 EP 1808176 A3 EP1808176 A3 EP 1808176A3 EP 07004317 A EP07004317 A EP 07004317A EP 07004317 A EP07004317 A EP 07004317A EP 1808176 A3 EP1808176 A3 EP 1808176A3
Authority
EP
European Patent Office
Prior art keywords
treatment
inflammation
reduced glucocorticoid
relates
glucocorticoid metabolites
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP07004317A
Other languages
German (de)
French (fr)
Other versions
EP1808176A2 (en
EP1808176B1 (en
Inventor
Brain Robert Walker
Ruth Andrew
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Edinburgh
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University of Edinburgh
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Publication date
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Publication of EP1808176A3 publication Critical patent/EP1808176A3/en
Application granted granted Critical
Publication of EP1808176B1 publication Critical patent/EP1808176B1/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/473Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/59Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Emergency Medicine (AREA)
  • Nutrition Science (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention relates to the modulation of glucocorticoid metabolism. In particular, the invention relates to the modulation of the functional activity of the glucocorticoid receptor by 5α reduced metabolic breakdown products of glucocorticoids. The invention relates to the treatment of inflammatory conditions in a patient.
EP07004317.9A 2002-06-14 2003-06-16 5 alpha reduced glucocorticoid metabolites for the treatment of inflammation Expired - Lifetime EP1808176B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0213745.3A GB0213745D0 (en) 2002-06-14 2002-06-14 Enzyme
EP03760087A EP1515718A2 (en) 2002-06-14 2003-06-16 Modulation of activation of glucocorticoid receptors by breakdown products of glucocorticoids

Related Parent Applications (2)

Application Number Title Priority Date Filing Date
EP03760087.1 Division 2003-06-16
EP03760087A Division EP1515718A2 (en) 2002-06-14 2003-06-16 Modulation of activation of glucocorticoid receptors by breakdown products of glucocorticoids

Publications (3)

Publication Number Publication Date
EP1808176A2 EP1808176A2 (en) 2007-07-18
EP1808176A3 true EP1808176A3 (en) 2007-12-26
EP1808176B1 EP1808176B1 (en) 2013-10-23

Family

ID=9938625

Family Applications (2)

Application Number Title Priority Date Filing Date
EP07004317.9A Expired - Lifetime EP1808176B1 (en) 2002-06-14 2003-06-16 5 alpha reduced glucocorticoid metabolites for the treatment of inflammation
EP03760087A Withdrawn EP1515718A2 (en) 2002-06-14 2003-06-16 Modulation of activation of glucocorticoid receptors by breakdown products of glucocorticoids

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP03760087A Withdrawn EP1515718A2 (en) 2002-06-14 2003-06-16 Modulation of activation of glucocorticoid receptors by breakdown products of glucocorticoids

Country Status (6)

Country Link
EP (2) EP1808176B1 (en)
JP (1) JP2005533785A (en)
AU (1) AU2003250368A1 (en)
CA (1) CA2489312A1 (en)
GB (3) GB0213745D0 (en)
WO (1) WO2003105838A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7790706B2 (en) 2002-06-14 2010-09-07 The University Of Edinburgh Treatment of inflammation with 5α reduced metabolites
WO2005027901A1 (en) * 2003-09-25 2005-03-31 Tel Aviv University Future Technology Development L.P. Compositions and methods using same for treating amyloid-associated diseases
EP2305352A1 (en) * 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
PT3206692T (en) * 2014-10-15 2024-04-30 Corcept Therapeutics Inc Fatty liver disease treatment using glucocorticoid and mineralocorticoid receptor antagonists

Citations (2)

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US5358943A (en) * 1987-12-29 1994-10-25 Clark Abbot F Use of tetrahydrocortisol to prevent elevations in intraocular pressure caused by corticosteroids
WO2003059267A2 (en) * 2001-12-21 2003-07-24 Rhode Island Hospital SELECTIVE 11β-HSD INHIBITORS AND METHODS FOR USE THEREOF

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AU634186B2 (en) 1988-11-11 1993-02-18 Medical Research Council Single domain ligands, receptors comprising said ligands, methods for their production, and use of said ligands and receptors
IL162181A (en) 1988-12-28 2006-04-10 Pdl Biopharma Inc A method of producing humanized immunoglubulin, and polynucleotides encoding the same
AU732820B2 (en) 1995-06-02 2001-05-03 Nexstar Pharmaceuticals, Inc. High-affinity oligonucleotide ligands to growth factors
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
JPH08259465A (en) * 1995-03-27 1996-10-08 Sekisui Chem Co Ltd External preparation for treating skin desease
JPH11513711A (en) * 1995-10-23 1999-11-24 メルク エンド カンパニー インコーポレーテッド 17-alkyl-7-substituted-4-azasteroid derivatives
US5939069A (en) * 1996-08-23 1999-08-17 University Of Florida Materials and methods for detection and treatment of immune system dysfunctions
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WO2003059267A2 (en) * 2001-12-21 2003-07-24 Rhode Island Hospital SELECTIVE 11β-HSD INHIBITORS AND METHODS FOR USE THEREOF

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BERGER T S ET AL: "INTERACTION OF GLUCOCORTICOID ANALOGUES WITH THE HUMAN GLUCOCORTICOID RECEPTOR", JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, vol. 41, no. 3-8, 1992, 10TH INTERNATIONAL SYMPOSIUM ON RECENT ADVANCES IN STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY, PARIS, pages 733 - 738, XP009024951, ISSN: 0960-0760 *
COLVILLE-NASH PAUL R ET AL: "The pharmacological modulation of angiogenesis in chronic granulomatous inflammation", JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol. 274, no. 3, 1995, pages 1463 - 1472, XP009024952, ISSN: 0022-3565 *
DUBROVSKY B ET AL: "EFFECTS OF CORTICOSTERONE AND 5-ALPHA DIHYDROCORTICOSTERONE ON BRAIN EXCITABILITY IN THE RAT", JOURNAL OF NEUROSCIENCE RESEARCH, vol. 14, no. 1, 1985, pages 117 - 128, XP009025027, ISSN: 0360-4012 *
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Also Published As

Publication number Publication date
EP1808176A2 (en) 2007-07-18
GB2426451A (en) 2006-11-29
GB0610137D0 (en) 2006-06-28
WO2003105838A2 (en) 2003-12-24
GB0213745D0 (en) 2002-07-24
JP2005533785A (en) 2005-11-10
CA2489312A1 (en) 2003-12-24
GB2407502A (en) 2005-05-04
EP1808176B1 (en) 2013-10-23
GB0500686D0 (en) 2005-02-23
AU2003250368A1 (en) 2003-12-31
WO2003105838A3 (en) 2004-05-06
EP1515718A2 (en) 2005-03-23

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